luotonin-a has been researched along with vasicinone* in 1 studies
1 other study(ies) available for luotonin-a and vasicinone
| Article | Year |
|---|---|
Design and synthesis of C-aryl angular luotonins via a one-pot aza-Nazarov-Friedlander sequence and their Topo-I inhibition studies along with C-aryl vasicinones and luotonins.
A facile one-pot synthesis of C-ring substituted angular luotonins has been realized via a methanesulfonic acid mediated aza-Nazarov-Friedlander condensation sequence on quinazolinonyl enones. Topoisomerase I (topo-I) inhibition studies revealed that the angular luotonin library (7a-7l) and their regioisomeric analogs (linear luotonins, 8a-8l) are weak negative modulators, compared to camptothecin. These results would fare well for the design of topo-I-inert luotonins for non-oncological applications such as anti-fungal and insecticide lead developments. Surprisingly, the tricyclic vasicinones (9h, 9i, and 9j) showed better topo-I inhibition compared to pentacyclic C-aryl luotonins providing a novel pharmacophore for further explorations. Topics: Alkaloids; DNA Topoisomerases, Type I; Dose-Response Relationship, Drug; Drug Design; Humans; Molecular Structure; Pyrroles; Quinones; Structure-Activity Relationship; Topoisomerase I Inhibitors | 2021 |